glutethimide
Trade name: doriden
Small moleculeapproved
Approved
Apr 16, 1957
Glutethimide is a GABA agonist that was introduced by Ciba in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similarly severe withdrawal symptoms. Glutethimide was discontinued in the US by manufacturers in 1993. Current production levels in the United States point to it only being used in small-scale research. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 7 marketing orgs
Phase 1
0
Phase 2
0
Phase 3
0
Phase 4
0
Timeline
1950s
- Apr 16, 1957
Sanofi-Aventis — Earliest FDA Approval
- Apr 16, 1957
Sanofi-Aventis — NDA Secondary Org
- Apr 16, 1957
Sanofi-Aventis — NDA Organization
1970s
- Oct 28, 1976
Upsher-Smith Laboratories — Marketing Organization
- Apr 1, 1977
Lannett Company, Inc. — Marketing Organization
- Aug 1, 1977
Watson Pharmaceuticals — Marketing Organization
Indications
Mechanism of action
- GABA-A receptor; anion channelPOSITIVE MODULATOR
GABA-A receptor; anion channel positive modulator
Likely allosteric but unclear whether benzodiazepine or barbiturate site involved
- Gamma-aminobutyric acid receptor subunit alpha-1 (GABRA1) ↗
- Gamma-aminobutyric acid receptor subunit beta-2 (GABRB2) ↗
- Gamma-aminobutyric acid receptor subunit gamma-2 (GABRG2) ↗
- Gamma-aminobutyric acid receptor subunit beta-3 (GABRB3) ↗
- Gamma-aminobutyric acid receptor subunit alpha-4 (GABRA4) ↗
- Gamma-aminobutyric acid receptor subunit gamma-3 (GABRG3) ↗
- Gamma-aminobutyric acid receptor subunit theta (GABRQ) ↗
- Gamma-aminobutyric acid receptor subunit alpha-3 (GABRA3) ↗
- Gamma-aminobutyric acid receptor subunit pi (GABRP) ↗
- Gamma-aminobutyric acid receptor subunit delta (GABRD) ↗
- Gamma-aminobutyric acid receptor subunit gamma-1 (GABRG1) ↗
- Gamma-aminobutyric acid receptor subunit beta-1 (GABRB1) ↗
- Gamma-aminobutyric acid receptor subunit epsilon (GABRE) ↗
- Gamma-aminobutyric acid receptor subunit alpha-2 (GABRA2) ↗
- Gamma-aminobutyric acid receptor subunit alpha-5 (GABRA5) ↗
- Gamma-aminobutyric acid receptor subunit alpha-6 (GABRA6) ↗
- GABA receptor alpha-1 subunit
- GABA receptor beta-2 subunit
- GABA receptor alpha-4 subunit
- GABA receptor delta subunit
- GABA receptor alpha-5 subunit
- GABA receptor alpha-6 subunit
- GABA receptor beta-3 subunit
- GABA receptor alpha-3 subunit
- GABA receptor alpha-2 subunit
- GABA-A receptor; GABA-A site (alpha1/beta2 interface)
- GABA-A receptor; alpha-3/beta-3/gamma-2
- GABA-A receptor; alpha-1/beta-3/gamma-2
- GABA-A receptor; alpha-5/beta-3/gamma-2
- GABA-A receptor; alpha-2/beta-3/gamma-2
- GABA-A receptor; alpha-1/beta-2/gamma-2
- GABA-A receptor; alpha-6/beta-3/gamma-2
- GABA-A receptor; benzodiazepine site
- GABA-A receptor; agonist GABA site
- GABA A receptor alpha-2/beta-2/gamma-2
- GABA A receptor alpha-3/beta-2/gamma-2
- GABA A receptor alpha-6/beta-2/gamma-2
- GABA A receptor alpha-1/beta-1/gamma-2
- GABA A receptor alpha-4/beta-3/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta3/delta
- Gamma-aminobutyric acid receptor subunit alpha-1/ beta-1
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-2
- Gamma-aminobutyric acid receptor subunit alpha-3/ beta-3/gamma-3
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-3/beta-3/theta
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3/gamma-3
- Gamma-aminobutyric acid receptor subunit alpha-6/beta-3
- GABA-A receptor alpha-1/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-1/beta-2/delta
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/delta
- Gamma-aminobutyric acid receptor subunit beta-1/beta-2
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-3
- Gamma-aminobutyric acid receptor subunit alpha-1/alpha-2/beta-2/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-1/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-2/gamma-2
- Gamma-aminobutyric acid receptor subunit alpha-4/beta-1/delta
- Gamma-aminobutyric acid receptor subunit alpha-5/beta-2/gamma-2
- GABA receptor beta-1 subunit
- Gamma-aminobutyric acid receptor subunit alpha-2/beta-1/gamma-2
Approval history
- approvedPriority reviewApr 16, 1957
Chemistry & pharmacology
Loading structure…
SMILES
CCC1(CCC(=O)NC1=O)C2=CC=CC=C2- Mol. weight
- 217.2637 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- Yes
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Discontinued
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaGlutethimide ↗
- NCATSC8I4BVN78E ↗
- ChEMBLCHEMBL1102 ↗
Also known as
- 2-ethyl-2-phenylglutarimide
- 2-ethyl-2-phenylglutarimide
- doriden
- doriden
- doriden
- doriden
- elrodorm
- glimid
- glutethimid
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutethimide
- glutetimid
- noxiron
- noxyron
- sarodormin
Organizations
Marketing (8)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Halsey | For profit | MKTG | Oct 10, 1986 |
| Lannett Company, Inc. | For profit | MKTG | Apr 1, 1977 |
| Sanofi-Aventis | For profit | NDA2 | Apr 16, 1957 |
| Sanofi-Aventis | For profit | NDA | Apr 16, 1957 |
| UCB | For profit | MKTG | — |
| Upsher-Smith Laboratories | For profit | MKTG | Oct 28, 1976 |
| Vitarine | For profit | MKTG | Apr 20, 1981 |
| Watson Pharmaceuticals | For profit | MKTG | Aug 1, 1977 |